| 王焕南,白波,陈京.G蛋白偶联受体磷酸化研究进展[J].济宁医学院学报,2016,39(6):416-420 |
| G蛋白偶联受体磷酸化研究进展 |
| Advances in G protein-coupled receptor phosphorylation |
| 投稿时间：2016-10-13 |
| DOI：10.3969/j.issn.1000-9760.2016.06.010 |
| 中文关键词: G蛋白偶联受体;磷酸化;信号转导;生物发光共振能量转移;Duolink |
| 英文关键词: G protein-coupled receptor;Phosphorylation;Signal transduction;Bioluminescence resonance energy transfer;Duolink |
| 基金项目:国家自然科学基金（31271243）；山东省自然科学基金（ZR2015CL021）；山东省高校科技计划（JY2015KJ001） |
|
| 摘要点击次数: 6512 |
| 全文下载次数: 1387 |
| 中文摘要: |
| G蛋白偶联受体（G protein-coupled receptors，GPCR）是具有重要生理病理功能的跨膜受体蛋白。GPCR磷酸化与G蛋白偶联受体激酶（G protein-coupled receptor kinases，GRKs）、蛋白激酶C（proteinkinase C，PKC）及β抑制蛋白（β-arrestin）密切相关。GPCR发生磷酸化可选择性的激活G蛋白依赖或G蛋白非依赖β-arresin信号转导通路，因而表现出偏向性受体/配体的特点。生物发光共振能量转移（bioluminescence resonance energy transfer，BRET）及Duolink等新技术的应用，推进了GPCR磷酸化的研究进程。本文简要综述了GRK、β-arrestin、PKC等对GPCR磷酸化的作用及GPCR发生磷酸化后对偏向性信号转导的影响，并探讨了目前研究GPCR磷酸化的最新技术，为进一步了解GPCR生理病理功能和药物研发提供理论基础。 |
| 英文摘要: |
| G protein-coupled receptors (GPCRs) are transmembrane proteins with important pathological and physiological functions.G protein-coupled receptor kinases (GRKs),protein kinase C (PKC) and β-arrestin are closely related to G protein-coupled receptor phosphorylation.The process of GPCR phosphorylation selectively activates G protein-dependent or G-protein-independent signal transduction pathways,which shows the characteristics of the biased receptor/ligand.In addition,new technologies,such as bioluminescence resonance energy transfer and Duolink etc.,furtherly promote the research of GPCRs phosphorylation.In this review,the effects of GRK,β-arrestin and PKC on the phosphorylation of GPCR and phosphorylation of GPCR were summarized.The application of newly found technologys in GPCR phosphorylation were also discussed,which provides a theoretical foundation to further understand GPCR physiological and pathological function and drug development. |
|
查看全文
查看/发表评论 下载PDF阅读器 |
